Background: Diabetes mellitus and concomitant dyslipidemia, being referred to as ‘diabetic
dyslipidemia’, are the foremost detrimental factors documented to play a pivotal role in cardiovascular
illness. Diabetic dyslipidemia is associated with insulin resistance, high plasma triglyceride levels, low
HDL-cholesterol concentration and elevated small dense LDL-cholesterol particles. Maintaining an
optimal glucose and lipid levels in patients afflicted with diabetic dyslipidemia could be a major task
that might require a well-planned diet-management system and regular physical activity, or otherwise
an intake of combined antidiabetic and antihyperlipidemic medications. Synchronized treatment which
efficiently controls insulin resistance-associated diabetes mellitus and co-existing dyslipidemia could
indeed be a fascinating therapeutic option in the management of diabetic dyslipidemia. Peroxisome
proliferator-activated receptors α/γ (PPARα/γ) dual agonists are such kind of drugs which possess
therapeutic potentials to treat diabetic dyslipidemia. Nevertheless, PPARα/γ dual agonists like muraglitazar,
naveglitazar, tesaglitazar, ragaglitazar and aleglitazar have been reported to have undesirable
adverse effects, and their developments have been halted at various stages. On the other hand, a recently
introduced PPARα/γ dual agonist, saroglitazar is an emerging therapeutic agent of glitazar class approved
in India for the management of diabetic dyslipidemia, and its treatment has been reported to be
generally safe and well tolerated.
Conclusion: Some additional and new compounds, at initial and preclinical stages, have been recently
reported to possess PPARα/γ dual agonistic potentials with considerable therapeutic efficacy and reduced
adverse profile. This review sheds light on the current status of various PPARα/γ dual agonists
for the management of diabetic dyslipidemia.